3-Substituted-2-(heteroaryl) indoles

Details 3-Substituted-2-(heteroaryl) indoles 3-Substituted-2-(heteroaryl) indoles

1983-05-17

1985-04-16

Fan, Jane T.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

546273, 546270, 548336, 514339, 514397, A61K 3144, C07D40104, C07D40304

Patent

active

045115737

ABSTRACT:
Disclosed as thromboxane synthetase inhibitors are the compounds of formula ##STR1## wherein R.sub.1 represents hydrogen or lower alkyl;
Ar represents 3-pyridyl or 1-imidazolyl, each unsubstituted or substituted by lower alkyl, carboxy, lower alkoxycarbonyl or carbamoyl;
R.sub.2 and R.sub.3 independently represent hydrogen, lower alkyl, halogen, trifluoromethyl, hydroxy, lower alkoxy, carboxy lower alkyl, lower alkoxycarbonyl lower alkyl, carboxy, lower alkoxycarbonyl, or lower alkyl-(thio, sulfinyl or sulfonyl), or R.sub.2 and R.sub.3 together on adjacent carbon atoms represent lower alkylenedioxy;
A represents straight chain or branched alkylene of 3 to 12 carbon atoms in which the number of the carbon atoms separating the indole nucleus from group B is 3 to 12, straight chain or branched alkenylene of 2 to 12 carbon atoms, straight chain or branched alkynylene of 2 to 12 carbon atoms, lower alkylenephenylene-lower (alkylene or alkenylene), lower alkylenephenylene, lower alkylene-(thio or oxy)-lower alkylene, lower alkylene-(thio or oxy)-phenylene, or lower alkylene-phenylene-(thio or oxy)-lower alkylene;
B represents carboxy, esterified carboxy, carbamoyl, mono- or di-lower alkylcarbamoyl, hydroxymethyl, cyano, hydroxycarbamoyl, 5-tetrazolyl or formyl; the imidazolyl and pyridyl N-oxide thereof; or a pharmaceutically acceptable salt thereof; as well as their synthesis, pharmaceutical compositions thereof, and methods of treatment utilizing such compounds.

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